US10039837B2ActiveUtilityA1
Multi-arm polyethylene glycol-azido derivative
Est. expiryDec 2, 2033(~7.4 yrs left)· nominal 20-yr term from priority
C08G 65/33396C08G 65/337C08G 65/33327C08G 65/332C08G 65/33337A61K 47/60C08G 65/3346C08G 65/333C08G 2650/30C08G 65/33331C08G 65/325A61K 47/48215
48
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Claims
Abstract
Provided is a multi-arm polyethylene glycol-azido derivative of general formula I, wherein R is a central molecule, which is selected from a polyhydroxy structure, a polyamino structure or a polycarboxyl structure; n is the number of branches or arms, n≥3; PEG is the same or different —(CH 2 CH 2 O) m —, the average value of m being an integer from 3 to 250; X is a linking group of a azido end group; k is the number of the branches having the azido end group; F is selected from the group consisting of amino, carboxyl, sulfhydryl, ester group, maleic imide group and acrylic group; and Y is a linking group of an end group F.
Claims
exact text as granted — not AI-modifiedThe invention claimed is:
1. A multi-arm polyethylene glycol-adizo derivative having a structure of a general formula I:
wherein:
R is a central molecule and R is pentaerythritol or polypentaerythritol structure, methyl glucoside, sucrose, glycerol or polyglycerol structure;
n is the number of branches or the number of arms, n≥3;
PEG is the same or different —(CH 2 CH 2 O) m —, m is an integer of average value of 3-250;
X is a linking group of a azido end group, selected from the group consisting of C 1-12 alkyl, aryl alkyl, ester group, carbonate group, amide group, amide ester group, ether group, urethane group;
k is the number of the branches having the azido end group, 2≤k≤n;
F is an active end group different from the azido, selected from the group consisting of amino, carboxyl, sulfhydryl, ester group, maleic imide group and acrylic group;
Y is a linking group of an end group F, selected from the group consisting of (CH 2 ) i , (CH 2 ) i NH, (CH 2 ) i OCOO—, (CH 2 ) i OCONH—, (CH 2 ) i NHCOO—, (CH 2 ) i NHCONH—, OC(CH 2 ) i COO—, (CH 2 ) i COO—, (CH 2 ) i CONH; i is an integer of 1-10.
2. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, the multi-arm polyethylene glycol-azido derivative having a structure of a general formula II:
R-|-PEG-X—N 3 ] k (II).
3. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, the multi-arm polyethylene glycol-azido derivative having a structure of a general formula III:
4. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, R is
wherein 1 is an integer of ≥1 and ≤10.
5. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, 3≤n≤22.
6. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, 3≤n≤6.
7. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, 2≤k≤16.
8. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, k is 2, 4, 6, 8, 10, 12, 14 or 16.
9. The multi-arm polyethylene glycol-adizo derivative of claim 4 , wherein, l is 1, 2, 3, 4, 5 or 6.
10. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, m is an integer of average value of 68-227.
11. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, X is selected from the group consisting of (CH 2 ) i , (CH 2 ) i NH, (CH 2 ) i OCOO—, (CH 2 ) i OCONH—, (CH 2 ) i NHCOO—, (CH 2 ) i NHCONH—, OC(CH 2 ) i COO—, (CH 2 ) i COO—, (CH 2 ) i CONH, (CH 2 ) i COO—.
12. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, Y is selected from the group consisting of (CH 2 ) i , (CH 2 ) i NH, (CH 2 ) i COO—, (CH 2 ) i CO—.
13. The multi-arm polyethylene glycol-adizo derivative of claim 11 , wherein, i is 1, 2, 3, 4 or 5.
14. The multi-arm polyethylene glycol-adizo derivative of claim 12 , wherein, i is 1, 2, 3, 4 or 5.
15. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, F is —NH 2 , —COOH, —OCH 3 ,
16. The multi-arm polyethylene glycol-adizo derivative of claim 1 , wherein, the multi-arm polyethylene glycol-adizo derivative is shown as:
17. A multi-arm polyethylene glycol-adizo derivative, wherein, the multi-arm polyethylene glycol-adizo derivative having a structure of following general formula:
wherein,
l is 1, 2, 3, 4, 5 or 6;
X is a linking group of an azido end group, selected from the group consisting of C 1-12 alkyl, aryl alkyl, ester group, carbonate group, amide group, amide ester group, ether group, urethane group.
18. A multi-arm polyethylene glycol-adizo derivative, wherein, the multi-arm polyethylene glycol-adizo derivative having a structure of following general formula:
wherein,
l is 1, 2, 3, 4, 5 or 6;
X is a linking group of an azido end group, selected from the group consisting of C 1-12 alkyl, aryl alkyl, ester group, carbonate group, amide group, amide ester group, ether group, urethane group.Cited by (0)
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